| 货号 | 10006426-50mg |
| 描述 | HDM-2 (human double minute-2; MDM-2 in mouse) is a key negative regulator of p53 that binds to and targets p53 for proteasomal degradation. Overexpression of HDM-2 in some tumors leads to inactivation of p53 thereby allowing tumor cells to escape p53-induced apoptosis.1 RITA (reactivation of p53 and induction of tumor cell apoptosis) is a small molecule inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53.2 It binds to p53 with an apparent Kd of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation and activation.2 RITA potently inhibits the growth of a variety of cancer cell lines in the sub-micromolar range, inducing both DNA-protein and DNA-DNA cross links in human renal cancer cells.3 RITA reduced tumor size by 90% at a dose of 10 mg/kg in SCID mice bearing HCT116 tumors, and caused complete regression of A-498 tumor cell xenografts in nude mice at a dose of 45 mg/kg.2,4 |
| 别名 | 2,5-bis(5-hydroxymethyl-2-thienyl) Furan;NSC 652287; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Chène, P. Inhibiting the p53-MDM2 interaction: An important target for cancer therapy. Nature Reviews.Cancer 3, 102-109 (2003). 2.Issaeva, N.,Bozko, P.,Enge, M., et al. Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activities p53 function in tumors. Nature Medicine 10(12), 1321-1328 (2004). 3.Nieves-Neira, W.,Rivera, M.I.,Kohlhagen, G., et al. DNA protein cross-links produced by NSC 652287, a novel thiophene derivate active against human renal cancer cells. Molecular Pharmacology 56, 478-484 (1999). 4.Rivera, M.I.,Stinson, S.F.,Vistica, D.T., et al. Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines. Differential accumulation and metabolism. Biochemical Pharmacology 57, 1283-1295 (1999). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 292.4 |
| 分子式 | C14H12O3S2 |
| CAS号 | 213261-59-7 |
| 稳定性 | ≥ 2 years |
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